Glesatinib(Synonyms: MGCD265)

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Glesatinib (Synonyms: MGCD265)

Glesatinib (MGCD265) 是一种具有口服活性的，有效的 MET/SMO 双抑制剂。 Glesatinib 是一种酪氨酸激酶抑制剂，可拮抗非小细胞肺癌 (NSCLC) 中 P 糖蛋白介导的多药耐药性 (MDR)。

Glesatinib(Synonyms: MGCD265)

Glesatinib Chemical Structure

CAS No. : 936694-12-1

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Glesatinib 的其他形式现货产品:

Glesatinib hydrochloride

生物活性

Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC)[1][2].

IC50 & Target[1]

MET

 

体外研究
(In Vitro)

Glesatinib (MGCD265; 0.01-5 μM; for 72 hours) results in a dose-dependent inhibition of cancer cell growth and shows the low IC50 value of 0.08 μM on NSCLC H1299 cells[1].
Glesatinib (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in NSCLC H1299 cells[1].
Glesatinib has the cytotoxicity to P-gp overexpressing cancer cells KB-C2, SW620/Ad300, HEK293/ABCB1, and their parent cells KB-3-1, SW620, HEK293 cells with the IC50s fell between 5 and 10 μM[1].
Glesatinib (1, 3 μM; 120 mins) increases the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp[2].
Glesatinib (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: NSCLC H1299 cells
Concentration: 0.01, 0.1, 1, 2, 5 μM
Incubation Time: For 72 hours
Result: Resulted in a dose-dependent inhibition of cancer cell growth and showed the lowest IC50 value of 0.08 μM.

体内研究
(In Vivo)

Glesatinib (MGCD265; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 4−6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts[1]
Dosage: 15 mg/kg
Administration: Orally; daily; 40 weeks
Result: Caused a significant decrease in tumor size.

Clinical Trial

分子量

619.70

Formula

C31H27F2N5O3S2
CAS 号

936694-12-1
中文名称

葛雷沙替尼
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Morgillo F, et al. Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. J Med Chem. 2017 Sep 14;60(17):7447-7458.

    [2]. Cui Q, et al. Glesatinib, a c-MET/SMO Dual Inhibitor, Antagonizes P-glycoprotein Mediated MultidrugResistance in Cancer Cells. Front Oncol. 2019 Apr 25;9:313.

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